Discovery of structurally novel, potent and orally efficacious GPR119 agonists
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Alper, Phillip and Epple, Robert (2014) Discovery of structurally novel, potent and orally efficacious GPR119 agonists. Bioorganic and Medicinal Chemistry Letters, 24 (10). pp. 2383-2387. ISSN 1464-3405
Abstract
Screening hit 5 was identified in a biochemical screen for GPR119 agonists. Compound 5 was structurally novel, displayed modest biochemical activity and no oral exposure, but was structurally distinct from typical GPR119 agonist scaffolds. Systematic optimization led to compound 36 with significantly improved in vitro activity and oral exposure, to elevate GLP1 acutely in an in vivo mouse model at a dose of 10 mg/kg. © 2014 Elsevier Ltd. All rights reserved.
Item Type: | Article |
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Keywords: | GPCR agonists GPR119 Pyrazolopyrimidines Type 2 diabetes |
Date Deposited: | 14 Mar 2018 00:45 |
Last Modified: | 25 Jan 2019 00:46 |
URI: | https://oak.novartis.com/id/eprint/11041 |